Rationally Designed, Conformationally Constrained Inverse Agonists of RORγt—Identification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy

Author:

Marcoux David1ORCID,Duan James J.-W.1ORCID,Shi Qing1ORCID,Cherney Robert J.1,Srivastava Anurag S.1,Cornelius Lyndon1,Batt Douglas G.1,Liu Qingjie1,Beaudoin-Bertrand Myra1,Weigelt Carolyn A.1,Khandelwal Purnima1,Vishwakrishnan Sureshbabu2,Selvakumar Kumaravel2,Karmakar Ananta2ORCID,Gupta Arun Kumar2,Basha Mushkin2,Ramlingam Sridharan2,Manjunath Naveen2,Vanteru Sridhar2,Karmakar Sukhen2,Maddala Nageswara2,Vetrichelvan Muthalagu2ORCID,Gupta Anuradha2ORCID,Rampulla Richard A.1,Mathur Arvind1,Yip Shiuhang1,Li Peng1,Wu Dauh-Rurng1,Khan Javed1,Ruzanov Max1,Sack John S.1,Wang Jinhong1,Yarde Melissa1,Cvijic Mary Ellen1,Li Sha1,Shuster David J.1,Borowski Virna1,Xie Jenny H.1,McIntyre Kim W.1,Obermeier Mary T.1,Fura Aberra1,Stefanski Kevin1,Cornelius Georgia1,Hynes John1,Tino Joseph A.1,Macor John E.1,Salter-Cid Luisa1,Denton Rex1,Zhao Qihong1,Carter Percy H.1ORCID,Dhar T. G. Murali1ORCID

Affiliation:

1. Research and Development, Bristol-Myers Squibb, 3551 Lawrenceville Rd, Princeton, New Jersey 08540, United States

2. Department of Discovery Synthesis, Biocon Bristol-Myers Squibb Research Centre, Biocon Park, Bommasandra IV Phase, Jigani Link Road, Bengaluru 560099, India

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

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